DC11870 |
RORγt-IN-9a |
A potent, selective, CNS penetrant, orally bioavailable RORγt with pIC50 of 8.3 in FRET assays. |
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DC10955 |
CD12681 |
CD12681 (CD-12681) is a potent, selective RORγ inverse agonist with IC50 of 19 nM, displays no activity against a panel of nuclear receptors (RORα, RARγ, LXRβ, PPARγ and VDR). |
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DC11845 |
GNE-3500 |
GNE-3500 (GNE3500) is a potent, selective, and orally bioavailable RORγ inhibitor with IC50 of 47 nM in IL-17 promoter assays. |
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DC11189 |
GNE-6468 |
GNE-6468 (GNE6468) is a potent and selective RORc inverse agonist (EC50=2 nM) with >1,000-fold selectivity for RORc over PPARγ. |
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DC9713 |
GSK2981278
Featured
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GSK2981278 is a highly potent and selective inverse agonist of retinoic acid receptor-related orphan receptor gamma (ROR gamma). |
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DC11047 |
MRL871
Featured
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MRL-871 (MRL871) is a potent, selective inhibitor of RORγt via allosteric inverse agonism, inhibits coactivator binding with IC50 of 7 nM; significantly reduces the IL17a mRNA levels in EL4 murine lymphoblast cell line at 10 uM. |
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DCAPI1187 |
Nobiletin (Hexamethoxyflavone) |
Nobiletin (Hexamethoxyflavone) |
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DC11224 |
PF-06747711 |
PF-06747711 (PF06747711) is a potent, selective, orally bioavailable RORC2 (RORγt) inverse agonist with IC50 of 4.1 nM. |
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DC11054 |
RORγt inverse agonist 22 |
RORγt inverse agonist 22 is a potent, subtype selective RORγt inverse agonist with binding IC50 of 18 nM, displays >192-fold selectivity over RORα and RORβ. |
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DC11202 |
RORγt inverse agonist 32 |
RORγt inverse agonist 32 is a potent, orally bioavailable inverse agonist of RORγt with IC50 of 9 nM in SPA binding assays. |
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DC8096 |
SR1001 |
SR1001 is a high-affinity synthetic ligand of RORα and RORγ; suppresses TH17 cell differentiation and inhibits autoimmunity. |
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DC11046 |
SR2211
Featured
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SR2211 (SR-2211) is a potent, selective RORγ inverse agonist (Ki=105 nM, IC50=320 nM) that potently inhibits production of IL-17 in cells. |
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DC11846 |
TMP778
Featured
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TMP778 (TMP-778) is a potent, selective RORγt inhibitor with IC50 of 7 nM in FRET assays and 63 nM in IL-17 promoter assays, with no inverse agonist activity. |
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DC11844 |
VTP-43742 |
VTP-43742 (VTP43742) is a highly potent, selective, oral RORγt inverse agonist for the treatment of autoimmune disorders, including multiple sclerosis and psoriasis.. |
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DC11869 |
RORγt inhibitor 1 |
A potent, selective, orally bioavailable RORγt inverse agonist with IC50 of 17 nM in TR-FRET assays |
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DC28137 |
TMP780 |
TMP780 is an inverse agonist of RORγt with an IC50 of 13 nM. RORγt is a tractable drug target for the treatment of cutaneous inflammatory disorders. |
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DC28379 |
TMP920 |
TMP920 is a highly potent and selective RORγt antagonist. TMP920 inhibits RORγt binding to the SRC1 peptide with an IC50 of 0.03 μM. |
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DC28745 |
FM26
Featured
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FM26 (compound 25) is a potent and allosteric retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists with an IC50 of 264 nM. FM26 has a distinct isoxazole chemotype and effectively reduces IL-17a mRNA production in EL4 cells. |
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DC40046 |
Vimirogant hydrochloride |
Vimirogant (VTP-43742) hydrochloride is a potent, selective, and orally active RORγt inhibitor (Ki=3.5 nM; IC50=17 nM). Vimirogant hydrochloride exhibits >1000-fold selectivity versus the RORα and RORβ isotypes. Vimirogant hydrochloride inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC50=57 nM) without affecting Th1, Th2, or Treg cell differentiation. Vimirogant hydrochloride has the potential for autoimmune disorders research. |
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DC40965 |
BMS-986251
Featured
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BMS-986251 is an orally active and selective RORγt inverse agonist with an EC50 of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC50 of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced models (preclinical models of psoriasis).
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DC44171 |
RORγt Inverse agonist 6
Featured
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RORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the study of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo. |
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DC44172 |
RORγt inverse agonist 13
Featured
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RORγt inverse agonist 13 (Compound 3i) is a potent, orally active and selective RORγt inverse agonist, with improved drug-like properties, with an IC50 of 63.8 nM. |
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DC46880 |
Cedirogant
Featured
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Cedirogant (ABBV-157) is an orally active RORγt inverse agonist. Cedirogant can be used for psoriasis research. |
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DC47003 |
Bevurogant
Featured
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Bevurogant is a retinoid-related orphan receptor-gamma t (RORγt) antagonist. Bevurogant can be used for the research of chronic inflammatory diseases. |
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DC47345 |
RORγt inverse agonist 23 |
RORγt inverse agonist 23 is a potent, selective, and orally available novel retinoic acid receptor-related orphan receptor γt inverse agonist. |
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DC47346 |
RORγ agonist 1 |
RORγ agonist 1 is a potent and orally bioavailable RORγ agonist (EC50 = 21 nM) with antitumor activity. |
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DC47901 |
SHR168442 |
SHR168442 is a modulator of retinoid-related orphan receptor gamma (RORγ) with an IC50 value of 0.035 μM. |
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DC48272 |
Retezorogant |
Retezorogant is a retinoid-related orphan receptor γ (RORγ) antagonist, extracted from patent WO2016093342 A1. |
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DC48944 |
RORγt/DHODH-IN-3 |
RORγt/DHODH-IN-3 (compound (S)-14d) is a dual RORγt/DHODH inhibitor, with IC50s of 0.098 μM and 0.432 μM, respectively. RORγt/DHODH-IN-3 exhibits remarkable in vivo anti-inflammatory activity. |
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DC48945 |
RORγt/DHODH-IN-1 |
RORγt/DHODH-IN-1 (compound (R)-14d) is a potent and orally active dual RORγt/DHODH inhibitor, with IC50s of 0.083 μM and 0.172 μM, respectively. RORγt/DHODH-IN-1 exhibits remarkable in vivo anti-inflammatory activity. |
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